Microneedles and Their Application in Transdermal Delivery of Antihypertensive Drugs—A Review
Abstract
:1. Introduction
2. Overview of Hypertension
2.1. Hypertension and Different Treatment Strategies for Hypertension
2.2. Etiology and Risk Factors of Hypertension
2.3. Problems Concerning Oral Drug Administration of Antihypertensive Drugs
3. Overview and Classification of Microneedles
4. Fabrication and Current Status of Microneedles
4.1. Microneedle Design and Fabrication
Material | Fabrication Method | Comments | Advantage | Disadvantage | References |
---|---|---|---|---|---|
Metal | Drawing lithograph; lithography, electroplating and molding (LIGA); laser drilling; electrodeposition; photochemical etching; electroplating | Porous structure long microneedles causing pain during administration | Good mechanical properties, high fracture resistance, robust and difficult to break, biocompatible | Cause an allergic reaction, costly startup | [100,113,116] |
Silicon | Silicon deep reactive ion etching (DRIE); micromolding; Photolithography; LIGA (which uses deep X-ray lithography) | Better biocompatibility but brittle and prone to shatter in use | Desirable sizes that are sufficiently flexible to be manufactured | Fabrication takes a long time and is an expensive procedure and causes skin fractures | [100,113,117] |
Polymer | Casting; photolithography; micromolding; | Biocompatible polymers, painless microneedles | Outstanding biocompatibility, limited toxicity, and affordable | Limited strength of microneedles | [100,113,118] |
Ceramic | Micromolding; lithography | Transfers the geometric shape master pattern to the substrate’s surface | Exhibits resistance to chemicals and compression | Limited tension strength of microneedles | [100] |
4.1.1. Silicon MN Fabrication
4.1.2. Polymer MN Fabrication
4.2. Diverse Application of MNs in Advanced Drug Delivery
4.3. Mechanism, Pharmacokinetics, and Insertion Behavior of MNs
4.4. Advantages of MNs for Drug Delivery, Patient Monitoring, Diagnostics, and Vaccine Delivery
4.5. MN-Mediated Antihypertensive Agents and Some Reported Nanoparticle-Based Delivery Systems
4.5.1. Calcium Channel Blockers (CCB)
4.5.2. Angiotensin-Converting Enzyme Inhibitors (ACE)
4.5.3. Angiotensin II Receptor Antagonists (ARB)
4.5.4. β-Blockers
4.5.5. Diuretics
Drugs | Class | MN Type | BCS Drug Classification | Therapeutic Area | Comments | References |
---|---|---|---|---|---|---|
Captopril, metoprolol tartrate | ACE inhibitor and β-blocker | Stainless steel microneedle rollers and arrays | BCS class III, BCS class I | Hypertension | Significant enhancement in transdermal flux after the application of microneedle | [144] |
Sodium nitroprusside | Vasodilator | Dissolvable microneedle patch | - | Hypertension | Rapid and potent BP reduction was observed | [23] |
Propranolol hydrochloride | β-blocker | Dissolving microneedles | BCS class I | Infantile hemangioma | Significantly increased the permeability and skin retention, enhancing dermal delivery | [153] |
Diltiazem hydrochloride, perindopril erbumine | Calcium channel blocker and ACE inhibitor | Microneedle rollers | BCS class I, BCS class III | Hypertension | Increase in transdermal penetration by 113.59-fold | [1] |
Nifedipine, diltiazem | Calcium channel blocker | Bio-responsive microneedles | BCS class II and BCS class I | Hypertension | Significantly reduced the mean blood pressure, system co-delivers the drug | [141] |
Verapamil, amlodipine | Calcium channel blocker | Stainless steel solid microneedles and microneedle rollers | BCS class I for both | Hypertension | Increased percutaneous penetration | [139] |
Hydrophilic drugs (atenolol, sotalol) and lipophilic molecules (propranolol, acebutolol) | β-blockers | Microneedle-mediated iontophoretic delivery | BCS class III BCS class I BCS class I BCS class III | Increase permeation rate | [154] | |
Lisinopril dihydrate, atorvastatin, aspirin | ACE inhibitors, statins, salicylates | Microneedle arrays | BCS class I BCS class III BCS class II | Cardiovascular disease | Combined drug delivery from a single-dissolving MN array | [150] |
Amlodipine | Calcium channel blocker | Polymeric microneedle | BCS class I | Hypertension | Enhanced transdermal permeation | [140] |
Nicardipine hydrochloride | Calcium channel blocker | Solid microneedle | BCS class II | Hypertension | Improved transdermal delivery of nicardipine | [108] |
Amlodipine besylate | Calcium channel blocker | Hydrogel microneedle | BCS class I | Hypertension | Transdermal delivery of amlodipine in controlled manner | [142] |
Losartan potassium | Angiotensin receptor blocker | Polymeric microneedle | BCS class III | Hypertension | Improved transdermal delivery | [146] |
Losartan | Angiotensin receptor blocker | Dissolving microneedle patch | BCS class III | Skin disease | Enhanced drug delivery efficiency | [145] |
Valsartan | Angiotensin receptor blocker | Solid microneedle | BCS class II or III | Hypertension | Improved drug permeation and significant impact on hypertension | [147] |
Valsartan | Angiotensin receptor blocker | Solid microneedle | BCS class II or III | Hypertension | Enhanced drug permeation using combination of transdermal patch and microneedle | [148] |
Valsartan | Angiotensin receptor blocker | Solid microneedle | BCS class II or III | Hypertension | Improved bioavailability of valsartan | [149] |
Atenolol, bisoprolol | β-blockers | Stainless steel microneedles and gold titanium microneedle rollers | BCS class III BCS class I | Enhanced percutaneous penetration of drugs | [155] | |
Carvedilol | β-blockers | Microneedle | BCS class II | Hypertension | Improved bioavailability of carvedilol | [156] |
Furosemide | Loop diuretics | Polymeric microneedle | BCS class IV | Sustained release of furosemide | [158] |
4.6. MNs for the Transdermal Delivery of Hypertensive Drugs: Critical Attributes and Upcoming Challenges
4.7. MNs Bypass First-Pass Metabolism and High Variability in Drug Plasma Levels of Antihypertensive Drugs
4.8. Patents on MNs
5. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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Class | Drug | BCS Class | Metabolism | Solubility | t1/2 | Log P | Oral Bioavailability | References |
---|---|---|---|---|---|---|---|---|
Calcium channel blocker | Verapamil | BCS class I | Extensively metabolized by CYP2C8, CYP2C18, and CYP2C9 hepatic first-pass metabolism, | 7 mg/mL | 2–7 h | 3.8 | 10–20% | [31,51] |
Calcium channel blocker | Nifedipine | BCS class II drug | Hepatic metabolism by CYP3A4 high first pass metabolism | 20 µg/mL | 2 h | 2.20 | 45–56% | [31,51] |
Calcium channel blocker | Amlodipine | BCS class I | Extensive hepatic Metabolized by CYP3A4 | 75.3 µg/mL | 30–50 h | 2.22 | 64% | [31,51] |
Calcium channel blocker | Felodipine | BCS class II | Inclusively metabolized by CYP3A4 | 7.15 µg/mL | 7–21 h | 4.36 | 15% | [31,51] |
Angiotensin II receptor blocker | Valsartan | BCS class II | CYP2C9 | <0.1 mg/mL | 7.5 h | 5.8 | <25% | [51,52] |
Angiotensin II receptor blocker | Losartan | BCS class III | CYP2C9, CYP3A4 | 3.3 mg/mL | 1.5–2 h | 4.5 | 25–35% | [52,53,54] |
Angiotensin II receptor blocker | Telmisartan | BCS class II | CYP2C8, CYP2C9, and CYP2J2 | 9.9 μg/mL | 24 h | 7.7 | 42–58% | [55,56,57] |
Beta-blocker | Carvedilol | BCS class II | CYP1A2, CYP3A4, CYP1A1, CYP2D6, CYP2E1, CYP2C9 | 0.583 µg/mL | 7–10 h | 4.1 | 25–35% | [51,58,59] |
Beta-blocker | bupranolol | BCS class II | CYP2D6 first-pass metabolism (>90%) | - | 2–4 h | 2.9 | 10% | [59,60] |
Renin inhibitor | Aliskiren | BCS class III | CYP3A4- mediated hepatic metabolism | 122 mg/mL as salt | 24 h | 2.45 | 2.5% | [51,61] |
Angiotensin-converting enzyme inhibitor | Ramipril | BCS class I | Carboxylesterase | 3.5 mg/mL | 13–17 h | 0.92 | 55–65% | [52,62,63] |
Angiotensin-converting enzyme inhibitor | Captopril | BCS class III | - | 125–160 mg/mL | 1–3 h | 1.02 | 65% | [52,64] |
Angiotensin-converting enzyme inhibitor | Lisinopril | BCS class III | - | 0.45 mg/mL | 12 h | 1.2 | 25% | [52,65] |
Angiotensin-converting enzyme inhibitor | Enalapril | BCS class III | Carboxylesterase | - | 11–14 h | 0.19 | 40–60% | [52,62] |
Thiazide-like diuretics | Indapamide | BCS class II | CYP3A4 | - | 14 h | 2.52 | 100% | [52,62] |
Alpha-blocker | Terazosin | BCS class III | - | - | 12 h | 2–3 | Completely absorbed | [66,67,68] |
Alpha-blocker | Prazosin | BCS class II | - | 0.2–1.6 mg/mL | 2.9 h | 0.173 | 56.9% | [69,70,71,72] |
Vasodilators | Hydralazine | BCS class III | CYP1A2 | 2–7 h | 0.83 | 30–50% | [73,74,75] | |
Vasodilators | Minoxidil | BCS class II | - | 2.2 mg/mL | 4.2 h | 0.6 | 90% | [74,76] |
MN Type | Characteristics/Method of Delivery | Advantages | Disadvantages | Application | Material | References |
---|---|---|---|---|---|---|
Hollow microneedle | Control release of the drug throughout the time pressure drives the flow through needle | High dose of drug solution, proper materials used to attain hydrophilic behavior, constant flow rate, dose accuracy, easy to formulate | Needle design requires great care, to withstand flow pressure, require durable material for preparation, require prefilled syringes, blocking the narrow channels | Disease diagnosis | Silicon | [100,101,102,103] |
Coated microneedle | Low dose of the encapsulated drug, coating drug release | Rapid drug delivery through the skin, potent drugs requiring low doses increase the permeability of drugs, stability of drug, mechanical strength | Prone to infection and drug loss during fabrication, damaged needles irritate, expensive manufacturing method | Drug and vaccine delivery | Silicon | [100,103,104] |
Solid microneedle | Channels created in the skin cause drugs to penetrate the lowest layers of the skin, sharper tip, adequate mechanical strength | Allows more drugs to pass into the skin, easy to formulate, can be formulated from a range of materials, increase the permeability of drugs | To prevent the possibility of infections, microincisions required to be stitched up, fracture of micron-sized needles under the skin, restricted availability of drug surface area available | Drug delivery | Silicon Metal Polymer | [100,103,105,106] |
Dissolving microneedle | Macromolecules release rapidly, releasing the drug by dissolving under the skin | Ease of administration for patients, easy manufacturing | Requires technical expertise to manufacture, utilization of biodegradable materials, dissolving takes time | Drug and vaccine delivery | Polymer | [100,103,107,108] |
Porous microneedle | Loading of drug achieved by different pore sizes; during manufacturing, porosity can be achieved | Higher capability of drug loading, the simplest method employed for fabrication | Lower ability to penetrate the skin | Disease diagnosis | Stainless steel, Titanium | [109,110,111] |
Hydrogel | Sustained drug release achieved by a minimally invasive device | Significantly improved biocompatibility, biodegradability, tolerability, affordability, controlled release of drug | Lower mechanical strength | Drug delivery | Polymer | [110,111,112] |
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Khalid, R.; Mahmood, S.; Mohamed Sofian, Z.; Hilles, A.R.; Hashim, N.M.; Ge, Y. Microneedles and Their Application in Transdermal Delivery of Antihypertensive Drugs—A Review. Pharmaceutics 2023, 15, 2029. https://doi.org/10.3390/pharmaceutics15082029
Khalid R, Mahmood S, Mohamed Sofian Z, Hilles AR, Hashim NM, Ge Y. Microneedles and Their Application in Transdermal Delivery of Antihypertensive Drugs—A Review. Pharmaceutics. 2023; 15(8):2029. https://doi.org/10.3390/pharmaceutics15082029
Chicago/Turabian StyleKhalid, Ramsha, Syed Mahmood, Zarif Mohamed Sofian, Ayah R. Hilles, Najihah Mohd Hashim, and Yi Ge. 2023. "Microneedles and Their Application in Transdermal Delivery of Antihypertensive Drugs—A Review" Pharmaceutics 15, no. 8: 2029. https://doi.org/10.3390/pharmaceutics15082029